Estrogens and antiestrogens Flashcards
Natural estrogens
Estradiol > Estrone > Estriol
Estradiol, most potent, formed by ovaries
Estrone and Estriol are formed in the liver and adipose from androstenedione. androstenedione and DHEA made by adrenal cortex.
PreMarin- Pregnant Horse Estrogen Pregnant Marin (Mare)
Synthetic estrogens
Steroids:
- EthinylEstradiol
- Mestranol
- Quinestrol
Non-steroidal
- Dienestrol
- Methestrol
Conjugated, depot estyrogens
- Estradiol valerate
Steroidal estrogens
Ethinylestradiol
Mestranol
Quinestrol
What carrier is estrogen bound to in blood?
Sex hormone binding globulin
AND
Albumin
Clinical use for estrogen
Primary hypogonadism, hormone replacement; Turner syndrome
Postmenopausal hormone therapy along with progestins
Hormonal contraceptions
Ovarian suppression, dysmenorrhea, excessive bleeding, severe PMS
Hirsutism, Amenorrhea
Last line treatment for prostate cancer, a form of palliative chemical castration
Estrogen SEs
Increased risk for endometrial and breast cancers, hyperplasias.
Hypercoagulability
Nausea
Breast tenderness
Hyperpigmentation
Migraines
Cholestasis and gall stones
Hepatic adenomas
Postmenopausal uterine bleeding
What is Diethylstilbestrol?
A non-steroidal estrogen that is no longer used.
Was used in the 70’s
Daughters of mom’s who used DES have increased risk for infertility, ectopic pregnancies, and vaginal adenocarcinomas.
Estrogen contraindications
Endometrial or breast cancers
Endometriosis
Patients with undiagnosed genital bleeding (endometrial cancer?)
Severe liver disease (unable to process)
Thromboembolism history
Heavy smokers.
What are the SERMs
Clomifen Tamoxifen Toremifen Raloxifen Bazedoxifen
What are the aromatase inhibitors
Steroidal:
- Exemestane, Formestane
the steroidal aromatase inhibitors have androgenic effects in women.
Non-steroidal:
- Anastrozole
- Letrozole
- Fadrozole
